Organic and Medicinal Chemistry Letters
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Novel indole-bearing combretastatin analogues as tubulin polymerization inhibitors
Organic and Medicinal Chemistry Letters - Tập 3 - Trang 1-13 - 2013
The combretastatins are a class of natural stilbenoids. These molecules
generally share three common structural features: a trimethoxy "A"-ring, a
"B"-ring containing substituent often at C3′ and C4′, and an ethene bridge
between the two rings, which provides necessary structural rigidity. Members of
the combretastatin family possess varying ability to cause vascular disruption
in tumors. Combreta...
Four butyrolactones and diverse bioactive secondary metabolites from terrestrial Aspergillus flavipes MM2: isolation and structure determination
Organic and Medicinal Chemistry Letters - Tập 2 - Trang 1-8 - 2012
The chemical constituents and biological activities of the terrestrial
Aspergillus flavipes MM2 isolated from Egyptian rice hulls are reported. Seven
bioactive compounds were obtained, of which one sterol: ergosterol (1), four
butyrolactones: butyrolactone I (2), aspulvinone H (3), butyrolactone-V (6) and
4,4'-diydroxypulvinone (7), along with 6-methylsalicylic acid (4) and the
cyclopentenone anal...
Pathways of ion–molecular interactions of nucleogenic phenyl cations with the nucleophilic centers of picolines
Organic and Medicinal Chemistry Letters - - 2012
The nuclear-chemical method brought unique opportunity for synthesis of unknown
and hardly available organic compounds. Presence of tritium labeling allows
one-step preparation of radioactive markers for the investigation of chemical
and biological processes. The ion–molecular reactions of nucleogenic phenyl
cations with 4-picoline have been carried out. The phenyl cations were generated
by sponta...
Chemical characterization, antioxidant and inhibitory effects of some marine sponges against carbohydrate metabolizing enzymes
Organic and Medicinal Chemistry Letters - Tập 2 - Trang 1-12 - 2012
More than 15,000 marine products have been described up to now; Sponges are
champion producers, concerning the diversity of products that have been found.
Most bioactive compounds from sponges were classified into anti-inflammatory,
antitumor, immuno- or neurosurpressive, antiviral, antimalarial, antibiotic, or
antifouling. Evaluation of in vitro inhibitory effects of different extracts
from four ...
An efficient heterogeneous catalyst (CuO@ARF) for on-water C-S coupling reaction: an application to the synthesis of phenothiazine structural scaffold
Organic and Medicinal Chemistry Letters - Tập 4 - Trang 1-10 - 2014
Aryl sulfides have significant importance from biological and pharmaceutical
aspects. Transition metal-catalyzed carbon-sulfur cross-coupling reaction
represents an important tool for the synthesis of sulfides. Among various
transition metals, copper salts or oxides have found vast applicability. A
simple procedure for the preparation of poly-ionic amberlite resins embedded
with copper oxide nanop...
Facile synthesis of symmetrical bis(benzhydryl)ethers using p-toluenesulfonyl chloride under solvent-free conditions
Organic and Medicinal Chemistry Letters - Tập 3 - Trang 1-7 - 2013
The benzhydryl ether moiety is widely distributed in nature and constitutes a
key structural motif in numerous molecules of significant biological potential
and of prospective clinical uses. Solvent-free and cost-effective facile
synthesis of symmetrical bis(benzhydryl)ethers is, thus, much desirable. A
simple and efficient method for the facile synthesis of symmetrical
bis(benzhydryl)ethers direc...
Method development and validation of potent pyrimidine derivative by UV-VIS spectrophotometer
Organic and Medicinal Chemistry Letters - Tập 4 - Trang 1-6 - 2014
A rapid and sensitive ultraviolet-visible (UV-VIS) spectroscopic method was
developed for the estimation of pyrimidine derivative
6-Bromo-3-(6-(2,6-dichlorophenyl)-2-(morpolinomethylamino) pyrimidine4-yl)
-2H-chromen-2-one (BT10M) in bulk form. Pyrimidine derivative was monitored at
275 nm with UV detection, and there is no interference of diluents at 275 nm.
The method was found to be linear in t...
Assessing the pharmacokinetic profile of the CamMedNP natural products database: an in silico approach
Organic and Medicinal Chemistry Letters - Tập 3 - Trang 1-9 - 2013
Drug metabolism and pharmacokinetic (DMPK) assessment has come to occupy a place
of interest during the early stages of drug discovery today. Computer-based
methods are slowly gaining ground in this area and are often used as initial
tools to eliminate compounds likely to present uninteresting pharmacokinetic
profiles and unacceptable levels of toxicity from the list of potential drug
candidates, ...
Cannabinoid receptor type 2 (CB2)-selective N-aryl-oxadiazolyl-propionamides: synthesis, radiolabelling, molecular modelling and biological evaluation
Organic and Medicinal Chemistry Letters - Tập 2 - Trang 1-22 - 2012
The endocannabinoid system is involved in many physiological and pathological
processes. Two receptors (cannabinoid receptor type 1 (CB1) and type 2 (CB2))
are known so far. Many unwanted psychotic side effects of inhibitors of this
system can be addressed to the interaction with CB1. While CB1 is one of the
most abundant neuroreceptors, CB2 is expressed in the brain only at very low
levels. Thus,...
Synthesis and antileishmanial evaluation of some 2,3-disubstituted-4(3H)-quinazolinone derivatives
Organic and Medicinal Chemistry Letters - - 2014
Leishmaniasis is a neglected tropical parasitic diseases affecting millions of
people around the globe. Quinazolines are a group of compounds with diverse
pharmacological activities. Owing to their promising antileishmanial activities,
some 3-aryl-2-(substitutedstyryl)-4(3H)-quinazolinones were synthesized in good
yields (65.2% to 86.4%). The target compounds were synthesized by using
cyclization,...
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